Therapeutic Compounds and Uses Thereof

a technology of therapeutic compounds and compounds, applied in the field of therapeutic compounds and methods of treating proliferative diseases and diseases associated with anagiogenesis, can solve problems such as irreversible vision loss in developed countries

Active Publication Date: 2016-01-07
KALA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Benefits of technology

[0010]In another aspect, the present invention provides pharmaceutical compositions including a compound of Formula (I), or a pharmaceutically acceptable salt, solvate, hydrate, polymorph, co-crystal, tautomer, stereoisomer, isotopically labeled derivative, or prodrug thereof, and optionally a pharmaceutically acceptable carrier. In certain embodiments, the pharmaceutical compositions described herein include a therapeutically effective amount of a compound of Formula (I), or a pharmaceutically acceptable salt, solvate, hydrate, polymorph, co-crystal, tautomer, stereoisomer, isotopically labeled derivative, or prodrug t...

Problems solved by technology

Angiogenic ocular conditions represent the leading ...

Method used

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  • Therapeutic Compounds and Uses Thereof
  • Therapeutic Compounds and Uses Thereof
  • Therapeutic Compounds and Uses Thereof

Examples

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examples

[0173]In order that the invention described herein may be more fully understood, the following examples are set forth. It should be understood that these examples are for illustrative purposes only and are not to be construed as limiting this invention in any manner.

General Procedures

Compound 1

[0174]Free phenol (1 equiv) and potassium carbonate (5 equiv) were suspended in N,N-dimethylformamide. Benzyl bromide (I. equiv) was added dropwise and the reaction stirred at 45° C. for 2 hours. The solvent was evaporated and the remaining crust suspended in H2O. The slurry was sonicated and the solid filtered. Filter cake was washed with H2O and hexane, then dried under high vacuum. 1-I: Isolated as light brown solid, yield=1.7 g (95%), m / z 300 (M+H)+. 1-II: Obtained from a commercial source.

Compound 2

[0175]4-Amino-3-chlorophenol hydrochloride (1.1 to 1.5 equiv) was suspended in N,N-dimethylfomamide. The suspension was purged with nitrogen and sodium hydride (2 equiv, 60% suspension in oil)...

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Abstract

Described herein are compounds of Formula (I) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Methods of using the compounds or pharmaceutical compositions thereof for treating diseases are also provided.

Description

FIELD OF THE INVENTION[0001]This invention relates to therapeutic compounds and methods of treating proliferative diseases and diseases associated with anagiogenesis such as cancer and macular degeneration.BACKGROUND OF THE INVENTION[0002]Growth factors play an important role in angiogenesis, lymphangiogenesis, and vasculogenesis. Growth factors regulate angiogenesis in a variety of processes including embryonic development, wound healing, and several aspects of female reproductive function. Undesirable or pathological angiogenesis is associated with diseases including diabetic retinopathy, psoriasis, cancer, rheumatoid arthritis, atheroma, Kaposi's sarcoma, and hemangioma (Fan et al., 1995, Trends Pharmacol. Sci. 16: 57 66; Folkman, 1995, Nature Medicine 1: 27 31). Angiogenic ocular conditions represent the leading cause of irreversible vision loss in developed countries. In the United States, for example, retinopathy of prematurity, diabetic retinopathy, and age-related macular de...

Claims

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Application Information

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IPC IPC(8): C07D491/107C07D405/12C07D405/14C07D413/14
CPCC07D491/107C07D405/14C07D405/12C07D413/14
Inventor ONG, WINSTON ZAPANTANOWAK, PAWEL WOJCIECHASKEW, BEN C
Owner KALA PHARMA
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